Hirsjärvi Samuli, Peltonen Leena, Kainu Laura, Hirvonen Jouni
Division of Pharmaceutical Technology, Faculty of Pharmacy, PO Box 56, FIN-00014 University of Helsinki, Finland.
J Nanosci Nanotechnol. 2006 Sep-Oct;6(9-10):3110-7. doi: 10.1166/jnn.2006.439.
The chemical and physical stability of polymeric nanoparticles is poor in aqueous suspensions, and the drying of these particles is often problematic. In the present study, the stability of freeze-dried low molecular weight poly(L-lactic acid) (PLA) nanoparticles was enhanced by adding glucose and/or lactose to the formulation as cryo- and lyoprotectants, respectively. Also the effect of an extra stabilizer, Tween 80, was studied. The best freeze-dried PLA nanoparticle formulations were achieved, when glucose and lactose were added in combination so that the amount of lactose was double the amount of glucose. With this combination the redispersion of high-quality nanoparticles (homogenous particle dispersion with original size and without aggregates) was achieved. The addition of Tween 80 further improved the quality of freeze-dried PLA nanoparticles by facilitating the redispersion of the lyophilized cake into optimal nanoparticles.
聚合物纳米颗粒在水悬浮液中的化学和物理稳定性较差，并且这些颗粒的干燥往往存在问题。在本研究中，通过分别向制剂中添加葡萄糖和/或乳糖作为冷冻保护剂和冻干保护剂，提高了冻干的低分子量聚（L-乳酸）（PLA）纳米颗粒的稳定性。还研究了额外的稳定剂吐温80的作用。当葡萄糖和乳糖联合添加且乳糖量是葡萄糖量的两倍时，可获得最佳的冻干PLA纳米颗粒制剂。通过这种组合，实现了高质量纳米颗粒的再分散（具有原始尺寸且无聚集体的均匀颗粒分散体）。吐温80的添加通过促进冻干饼再分散为最佳纳米颗粒，进一步提高了冻干PLA纳米颗粒的质量。
